2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. PAK Apoptosis
  4. LCH-7749944

LCH-7749944  (Synonyms: GNF-PF-2356)

Cat. No.: HY-125035 Purity: 99.36%
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LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.

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LCH-7749944 Chemical Structure

LCH-7749944 Chemical Structure

CAS No. : 796888-12-5

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10 mM * 1 mL in DMSO
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Based on 4 publication(s) in Google Scholar

LCH-7749944 Related Antibodies

Top Publications Citing Use of Products

View All PAK Isoform Specific Products:

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

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Description

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].

IC50 & Target[1]

PAK4

14.93 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
7.7 μM
Compound: 23
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by Cell Titer-Glo assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by Cell Titer-Glo assay
[PMID: 28080063]
In Vitro

LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner[1].
LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells[1].
LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase[1].
LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LCH-7749944 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells
Concentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.

Apoptosis Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20 μM
Incubation Time: 12, 24, 48 hours
Result: Induced apoptosis of SGC7901 cells.

Cell Cycle Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20 μM
Incubation Time: 12, 24, 48 hours
Result: Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.

Western Blot Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20, 30 μM
Incubation Time: 24 hours
Result: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.
Molecular Weight

350.41

Formula

C20H22N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(NC2=NC(NCC3OCCC3)=C4C=CC=CC4=N2)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (713.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8538 mL 14.2690 mL 28.5380 mL
5 mM 0.5708 mL 2.8538 mL 5.7076 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8538 mL 14.2690 mL 28.5380 mL 71.3450 mL
5 mM 0.5708 mL 2.8538 mL 5.7076 mL 14.2690 mL
10 mM 0.2854 mL 1.4269 mL 2.8538 mL 7.1345 mL
15 mM 0.1903 mL 0.9513 mL 1.9025 mL 4.7563 mL
20 mM 0.1427 mL 0.7134 mL 1.4269 mL 3.5672 mL
25 mM 0.1142 mL 0.5708 mL 1.1415 mL 2.8538 mL
30 mM 0.0951 mL 0.4756 mL 0.9513 mL 2.3782 mL
40 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7836 mL
50 mM 0.0571 mL 0.2854 mL 0.5708 mL 1.4269 mL
60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1891 mL
80 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
100 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7134 mL
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LCH-7749944 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LCH-7749944796888-12-5GNF-PF-2356LCH7749944LCH 7749944PAKApoptosisp21 activated kinasesproliferationhumangastriccancercellsPAK4c-SrcEGFRcyclinD1Inhibitorinhibitorinhibit

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